Kanchan Devkota, Brian Lohse, Qing Liu
Jan 31, 2014
Citations
0
Influential Citations
32
Citations
Journal
ACS medicinal chemistry letters
Abstract
A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.